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Introduction: Differentiation between infection and sterile inflammation is one of the most difficult medical problems and is relevant in many clinical situations. Scintigraphy with radiolabeled antibiotics, especially labeled fluoroquinolones, is a promising tool for diagnosing bacterial inflammation. We have attempted to synthesize <sup>99m</sup>Tc-norfloxacin and studied its properties in experiment. Methods: In present study we labeled norfloxacin with 99mTc, determined its radiochemical purity by thin-layer chromatography procedure, compared the bactericidal activity of <sup>99m</sup>Tc-norfloxacin and unlabelled norfloxacin by disk diffusion, performed in vitro binding assays and evaluated the feasibility of <sup>99m</sup>Tc-norfloxacin to image soft-tissue infections in rat modal of thigh muscle infection. Scintigraphy was performed at 30 min, 90 min and 18 h post injection. Abscess -to-normal-site ratios were calculated. Results: In this study <sup>99m</sup>Tc-norfloxacin with high radiochemical purity and low colloid content was synthesized. Disk diffusion method showed that <sup>99m</sup>Tc-norfloxacin retains bactericidal properties of unlabelled norfloxacin. In vitro binding studies demonstrated small degree of the tracer binding with S. aureus and ability of <sup>99m</sup>Tc-norfloxacin to bind with killed as well as alive bacteria. Uptake of the tracer was clearly visible in infected muscles and not visible in sterile inflammed muscles. Conclusion: The <sup>99m</sup>Tc-norfloxacin retains bactericidal properties of unlabelled norfloxacin. The tracer demonstrated small degree of S. aureus binding both with killed as well as alive bacteria. Studies which were performed in vivo in rats with a model of thigh muscle infection showed good ability of the radiopharmaceutical to image the infection.
| Язык оригинала | Английский |
|---|---|
| Страницы (с-по) | 73-81 |
| Число страниц | 9 |
| Журнал | Iranian Journal of Nuclear Medicine |
| Том | 23 |
| Номер выпуска | 2 |
| Состояние | Опубликовано - 1 июн 2015 |
Отпечаток
ASJC Scopus subject areas
- Radiology Nuclear Medicine and imaging
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Synthesis and experimental study of norfloxacin labeled with technecium-99m as a potential agent for infection imaging. / Sazonova, Svetlana Ivanovna; Lishmanov, Yuriy Borisovich; Varlamova, Natalia Valerievna; Skuridin, Viktor Sergeevich; Ilushenkova, Yulia Nikolayevna; Karpova, Maria Rostislavovna; Nesterov, Evgeny Alexandrovich.
В: Iranian Journal of Nuclear Medicine, Том 23, № 2, 01.06.2015, стр. 73-81.Результат исследований: Материалы для журнала › Статья
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TY - JOUR
T1 - Synthesis and experimental study of norfloxacin labeled with technecium-99m as a potential agent for infection imaging
AU - Sazonova, Svetlana Ivanovna
AU - Lishmanov, Yuriy Borisovich
AU - Varlamova, Natalia Valerievna
AU - Skuridin, Viktor Sergeevich
AU - Ilushenkova, Yulia Nikolayevna
AU - Karpova, Maria Rostislavovna
AU - Nesterov, Evgeny Alexandrovich
PY - 2015/6/1
Y1 - 2015/6/1
N2 - Introduction: Differentiation between infection and sterile inflammation is one of the most difficult medical problems and is relevant in many clinical situations. Scintigraphy with radiolabeled antibiotics, especially labeled fluoroquinolones, is a promising tool for diagnosing bacterial inflammation. We have attempted to synthesize 99mTc-norfloxacin and studied its properties in experiment. Methods: In present study we labeled norfloxacin with 99mTc, determined its radiochemical purity by thin-layer chromatography procedure, compared the bactericidal activity of 99mTc-norfloxacin and unlabelled norfloxacin by disk diffusion, performed in vitro binding assays and evaluated the feasibility of 99mTc-norfloxacin to image soft-tissue infections in rat modal of thigh muscle infection. Scintigraphy was performed at 30 min, 90 min and 18 h post injection. Abscess -to-normal-site ratios were calculated. Results: In this study 99mTc-norfloxacin with high radiochemical purity and low colloid content was synthesized. Disk diffusion method showed that 99mTc-norfloxacin retains bactericidal properties of unlabelled norfloxacin. In vitro binding studies demonstrated small degree of the tracer binding with S. aureus and ability of 99mTc-norfloxacin to bind with killed as well as alive bacteria. Uptake of the tracer was clearly visible in infected muscles and not visible in sterile inflammed muscles. Conclusion: The 99mTc-norfloxacin retains bactericidal properties of unlabelled norfloxacin. The tracer demonstrated small degree of S. aureus binding both with killed as well as alive bacteria. Studies which were performed in vivo in rats with a model of thigh muscle infection showed good ability of the radiopharmaceutical to image the infection.
AB - Introduction: Differentiation between infection and sterile inflammation is one of the most difficult medical problems and is relevant in many clinical situations. Scintigraphy with radiolabeled antibiotics, especially labeled fluoroquinolones, is a promising tool for diagnosing bacterial inflammation. We have attempted to synthesize 99mTc-norfloxacin and studied its properties in experiment. Methods: In present study we labeled norfloxacin with 99mTc, determined its radiochemical purity by thin-layer chromatography procedure, compared the bactericidal activity of 99mTc-norfloxacin and unlabelled norfloxacin by disk diffusion, performed in vitro binding assays and evaluated the feasibility of 99mTc-norfloxacin to image soft-tissue infections in rat modal of thigh muscle infection. Scintigraphy was performed at 30 min, 90 min and 18 h post injection. Abscess -to-normal-site ratios were calculated. Results: In this study 99mTc-norfloxacin with high radiochemical purity and low colloid content was synthesized. Disk diffusion method showed that 99mTc-norfloxacin retains bactericidal properties of unlabelled norfloxacin. In vitro binding studies demonstrated small degree of the tracer binding with S. aureus and ability of 99mTc-norfloxacin to bind with killed as well as alive bacteria. Uptake of the tracer was clearly visible in infected muscles and not visible in sterile inflammed muscles. Conclusion: The 99mTc-norfloxacin retains bactericidal properties of unlabelled norfloxacin. The tracer demonstrated small degree of S. aureus binding both with killed as well as alive bacteria. Studies which were performed in vivo in rats with a model of thigh muscle infection showed good ability of the radiopharmaceutical to image the infection.
KW - Infection
KW - Inflammation
KW - Norfloxacin
KW - Scintigraphy
KW - Technecium-99m
UR - http://www.scopus.com/inward/record.url?scp=84938094736&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84938094736&partnerID=8YFLogxK
M3 - Article
AN - SCOPUS:84938094736
VL - 23
SP - 73
EP - 81
JO - Iranian Journal of Nuclear Medicine
JF - Iranian Journal of Nuclear Medicine
SN - 1681-2824
IS - 2
ER -